别孕烷醇酮

化合物

别孕烷醇酮(英语:allopregnanoloneALLO,也名为3α,5α-孕烷醇酮)是一种作用于大脑的神经甾体[2][3],可用于治疗产后抑郁症[3][4][5]

别孕烷醇酮
Skeletal formula of allopregnanolone
Ball-and-stick model of the allopregnanolone molecule
临床资料
商品名英语Drug nomenclatureZulresso
其他名称ALLO; Allo; ALLOP; AlloP; Brexanolone; SAGE-547; SGE-102; 5α-Pregnan-3α-ol-20-one; 3α-Hydroxy-5α-pregnan-20-one; 3α,5α-Tetrahydroprogesterone; 3α,5α-THP
给药途径Intravenous infusion[1]
药物类别英语Drug classNeurosteroids; Antidepressants
法律规范状态
法律规范
药物动力学数据
血浆蛋白结合率>99%[1]
药物代谢Non-CYP450 (keto-reduction via AKRs, glucuronidation via UGTs, sulfation via SULTs)[1]
生物半衰期9 hours[1]
排泄途径Feces: 47%[1]
Urine: 42%[1]
识别信息
  • 1-[(3R,5S,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone
    OR
    1-[(1S,2S,5R,7S,10R,11S,14S,15S)-5-hydroxy-2,15-dimethyltetracyclo[8.7.0.02,7.011,15]heptadec-14-yl]ethanone
CAS号516-54-1
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
化学信息
化学式C21H34O2
摩尔质量318.501 g/mol
3D模型(JSmol英语JSmol
  • CC(=O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC[C@@H]4[C@@]3(CC[C@H](C4)O)C)C
  • InChI=1S/C21H34O2/c1-13(22)17-6-7-18-16-5-4-14-12-15(23)8-10-20(14,2)19(16)9-11-21(17,18)3/h14-19,23H,4-12H2,1-3H3/t14-,15+,16-,17+,18-,19-,20-,21+/m0/s1
  • Key:AURFZBICLPNKBZ-SYBPFIFISA-N

参考文献

编辑
  1. ^ 1.0 1.1 1.2 1.3 1.4 1.5 存档副本 (PDF). [2019-05-26]. (原始内容存档 (PDF)于2020-11-12). 
  2. ^ Reddy DS. Neurosteroids: endogenous role in the human brain and therapeutic potentials. Progress in Brain Research 186. 2010: 113–37. ISBN 9780444536303. PMC 3139029 . PMID 21094889. doi:10.1016/B978-0-444-53630-3.00008-7.  |journal=被忽略 (帮助)
  3. ^ 3.0 3.1 Commissioner, Office of the. Press Announcements - FDA approves first treatment for post-partum depression. www.fda.gov. [21 March 2019]. (原始内容存档于2019-04-22) (英语). 
  4. ^ Frieder A, Fersh M, Hainline R, Deligiannidis KM. Pharmacotherapy of Postpartum Depression: Current Approaches and Novel Drug Development. CNS Drugs. March 2019, 33 (3): 265–282. PMID 30790145. doi:10.1007/s40263-019-00605-7. 
  5. ^ Wilkinson ST, Sanacora G. A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. Drug Discov. Today. February 2019, 24 (2): 606–615. PMID 30447328. doi:10.1016/j.drudis.2018.11.007.